- Photoredox-mediated C-H functionalization and coupling of tertiary aliphatic amines with 2-chloroazoles
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Herein, conditions for C-H functionalization of tertiary aliphatic amines and their subsequent coupling with a number of 2-chloroazole derivatives are reported. The reaction is facilitated by a catalytic amount of tris-fac-Ir(ppy)3, with blue light irradiation and takes place under mild and convenient conditions. Most couplings take place with excellent regioselectivity. The reaction is tolerant of a number of functional groups and allows for rapid access to α-azole carbinamines commonly found in post-translationally modified peptides.
- Singh, Anuradha,Arora, Amandeep,Weaver, Jimmie D.
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supporting information
p. 5390 - 5393
(2013/11/06)
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- HETEROCYCLIC AMINOBERBAMINE DERIVATIVES, THE PREPARATION PROCESS AND USE THEREOF
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The present invention relates to a novel berbamine derivative of formula I or a pharmaceutically acceptable salt thereof, a process for preparation of the same, a pharmaceutical composition comprising said compound and its use in manufacture of an antitumor medicament.
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Paragraph 0106
(2013/07/19)
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- Tuning and predicting biological affinity: Aryl nitriles as cysteine protease inhibitors
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A series of aryl nitrile-based ligands were prepared to investigate the effect of their electrophilicity on the affinity against the cysteine proteases rhodesain and human cathepsin L. Density functional theory calculations provided relative reactivities of the nitriles, enabling prediction of their biological affinity and cytotoxicity and a clear structure-activity relationship.
- Ehmke, Veronika,Quinsaat, Jose Enrico Q.,Rivera-Fuentes, Pablo,Heindl, Cornelia,Freymond, Céline,Rottmann, Matthias,Brun, Reto,Schirmeister, Tanja,Diederich, Fran?ois
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supporting information; experimental part
p. 5764 - 5768
(2012/08/28)
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- NUCLEAR TRANSPORT MODULATIORS AND USES THEREOF
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The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g
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Page/Page column 219-220
(2011/10/03)
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- Dihydropyrimidine Compounds and Their Uses in Preparation of Medicaments for Treating and Preventing Antiviral Diseases
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The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or
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Page/Page column 17
(2010/04/30)
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- DIHYDROPYRIMIDINE COMPOUNDS AND THEIR USES IN PREPARATION OF MEDICAMENTS FOR TREATING AND PREVENTING ANTIVIRAL DISEASES
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The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof, to a process for preparing the compound of formula (I), and to use of the compound of formula (I) or a pharmaceutically acceptable salt or hydrate thereof as a medicament, in particular as a medicament for the treatment and prevention of type B hepatitis.
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Page/Page column 25-26
(2009/04/23)
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- NOVEL PIPERAZINES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
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Disclosed are novel piperazine derivatives that act as agonists of the α7 nAChR. Also disclosed are phannaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
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Page/Page column 152
(2008/06/13)
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- EP2 RECEPTOR AGONISTS
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A compound of Formula (I) or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of Formulae (Ai), (Aii), (Aiii) D is selected from Formulae (Di), (Dii), (Diii), (Div), (Dv) B is selected from the group consisting of Formulae (Bi), (Bii), (Biii), (Biv) (Bv).
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Page/Page column 109
(2008/06/13)
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- MALONONITRILE COMPOUND AS PESTICIDES
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The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.
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Page/Page column 187-188
(2008/06/13)
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- 4-[(4-(CARBOXYETHYL) PIPERIDINYL) METHYL] PYRROLIDINES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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3-Substituted pyrrolidines having a 4-carboxypiperidinylmethyl substituent on the 4-position of the ring are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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- Fungicides for the control of take-all disease of plants
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A method of controlling Take-All disease of plants by applying a fungicide of the formula STR1 wherein Z1 and Z2 are C and are part of an aromatic ring which is benzothiophene; and A is selected from --C(X)-amine wherein the amine is an unsubstituted, monosubstituted or disubstituted amino radical, --C(O)--SR3, --NH--C(X)R4, and --C(=NR3)--XR7 ; B is --Wm --Q(R2)3 or selected from O-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R4 ; Q is C, Si, Ge, or Sn; W is --C(R3)p H(2-p) --; or when Q is C, W is selected from --C(R3)p H(2-p), --N(R3)m H(1-m)--, --S(O)p--, and --O--; X is 0 or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R and R2 is independently defined herein; R3 is C1 -C4 alkyl; R4 is C1 -C4 alkyl, haloalkyl, alkoxy, alkylthio, alkylamino, or dialkylamino; and R7 is C1 -C4 alkyl, haloalkyl, or phenyl, optionally substituted with halo, nitro, or R4 ; or an agronomic salt thereof.
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